Grossman Stuart A, Olson Jeffrey, Batchelor Tracy, Peereboom David, Lesser Glenn, Desideri Serena, Ye Xiaobu, Hammour Tarek, Supko Jeffrey G
NABTT CNS Consortium, 1550 Orleans Street, Baltimore, MD 21231, USA.
Neuro Oncol. 2008 Apr;10(2):190-8. doi: 10.1215/15228517-2007-055. Epub 2008 Feb 20.
Cyclooxygenase-2 (COX-2) expression has been linked to the prognosis, angiogenesis, and radiation sensitivity of many malignancies. Celecoxib, a selective COX-2 inhibitor, is predominantly eliminated by hepatic metabolism. This study was conducted to determine the effects of hepatic enzyme-inducing antiseizure drugs (EIASDs) on the pharmacokinetics of celecoxib. The safety of celecoxib administered with radiation for glioblastoma and the effect of the combined treatment on survival were also evaluated. Patients were stratified based on concomitant use of EIASDs. Celecoxib (400) mg was administered orally twice a day until tumor progression or dose-limiting toxicity. Standard radiation was administered without adjuvant chemotherapy. Sampling was performed to define the plasma concentration/time profile for the initial dose of celecoxib and steady-state trough concentrations. Thirty-five patients (22 +EIASD, 13 -EIASD) were enrolled. There were no significant differences in age, performance status, extent of surgery, or Mini Mental State Exam scores between the two cohorts. The treatment was well tolerated. All patients in the +EIASD arm were taking phenytoin. There were no significant differences in any celecoxib pharmacokinetic parameters between 15 +EIASD and 12 -EIASD patients. With 31 of 35 patients deceased, estimated median survival time for all patients was 12 months (+EIASD, 11.5 months; - EIASD, 16 months; p = 0.11). The pharmacokinetics of celecoxib is not significantly affected by the concomitant administration of phenytoin. Celecoxib administered during and after radiation is well tolerated. The potential difference in survival between the +EIASD and -EIASD groups deserves further evaluation.
环氧化酶-2(COX-2)的表达与许多恶性肿瘤的预后、血管生成及放射敏感性有关。塞来昔布是一种选择性COX-2抑制剂,主要通过肝脏代谢消除。本研究旨在确定肝酶诱导抗癫痫药物(EIASDs)对塞来昔布药代动力学的影响。还评估了塞来昔布联合放疗治疗胶质母细胞瘤的安全性及联合治疗对生存的影响。患者根据是否同时使用EIASDs进行分层。口服塞来昔布(400)mg,每日两次,直至肿瘤进展或出现剂量限制性毒性。在不进行辅助化疗的情况下给予标准放疗。进行采样以确定塞来昔布初始剂量的血浆浓度/时间曲线及稳态谷浓度。共纳入35例患者(22例同时使用EIASD,13例未使用EIASD)。两组患者在年龄、功能状态、手术范围或简易精神状态检查评分方面无显著差异。治疗耐受性良好。同时使用EIASD组的所有患者均服用苯妥英钠。15例同时使用EIASD的患者与12例未使用EIASD的患者在任何塞来昔布药代动力学参数上均无显著差异。35例患者中有31例死亡,所有患者的估计中位生存时间为12个月(同时使用EIASD组为11.5个月;未使用EIASD组为16个月;p = 0.11)。苯妥英钠的同时给药对塞来昔布的药代动力学无显著影响。放疗期间及放疗后给予塞来昔布耐受性良好。同时使用EIASD组与未使用EIASD组之间生存的潜在差异值得进一步评估。